Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 546/18)
  • Patent number: 5955470
    Abstract: This invention relates to novel amide derivatives of certain 2,6-methano-2H-quinolizine-type compounds, to the intermediates and processes for their preparation, to their ability to antagonize the effects of serotonin at the 5HT.sub.3 receptors, and to their end-use application in the treatment of chemotherapeutically-induced nausea and vomiting, as anti-anxiety agents, in the symptomatic treatment of pain associated with migraine, as anti-arrhythmic agents, in the treatment of cognitive disorders, in treating hallucinatory endogenous psychoses of the type manifested in patients suffering from schizophrenia, and mania, in the treatment of glaucoma, for stimulating gastric motility, to combat drug abuse, to treat sleep apnea and to treat irritable bowel syndrome.
    Type: Grant
    Filed: October 29, 1998
    Date of Patent: September 21, 1999
    Assignee: Merrell Pharmaceuticals, Inc.
    Inventor: Maurice W. Gittos
  • Patent number: 5932732
    Abstract: A process for preparing S type 2-substituted hydroxy-2-indolidinyl-butyric ester compound ?II!: ##STR1## wherein R.sup.o is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of "R"(in which the nitrogen atom is protected), R.sup.1 and R.sup.2 are lower alkyl group, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound ?I!: ##STR2## wherein the symbols are as defined above.
    Type: Grant
    Filed: October 28, 1997
    Date of Patent: August 3, 1999
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Takayuki Kawaguchi, Sumihiro Nomura, Kenji Tsujihara
  • Patent number: 5932587
    Abstract: The heterocyclic-fused pyridines are prepared by reaction of the corresponding heterocyclic-fused pyridine aldehydes with appropriately substituted Grignard or Wittig reagents. The heterocyclic-fused pyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of dislipidaemia and arteriosclerosis.
    Type: Grant
    Filed: June 27, 1997
    Date of Patent: August 3, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Carsten Schmeck, Matthias Muller-Gliemann, Gunter Schmidt, Arndt Brandes, Rolf Angerbauer, Michael Logers, Klaus-Dieter Bremm, Hilmar Bischoff, Delf Schmidt, Joachim Schuhmacher
  • Patent number: 5922875
    Abstract: A compound represented by the general formula (I) shown below ##STR1## or a pharmaceutically acceptable salt thereof can be used as the active ingredient in a pharmaceutical preparation. The pharmaceutical preparation is desirable for its anti-ulcer activity, for therapeutic use against tumors sustained by gastrin and other bioactive polypeptides correlated therewith, for therapeutic use in treating disorders of the gastrointestinal tract, for the treatment of pathological conditions of the central nervous system linked to imbalances in the neural physiological levels of gastrin or other bioactive polypeptides correlated therewith, for use in the treatment and prevention of pathological eye conditions caused by surgical treatment of cataracts or chronic ocular inflammation, and for the prevention of diseases of other sensory organs.
    Type: Grant
    Filed: December 29, 1997
    Date of Patent: July 13, 1999
    Assignee: Rotta Research Laboratorium S.p.A.
    Inventors: Francesco Makovec, Walter Peris, Lucio C. Rovati, Luigi A. Rovati
  • Patent number: 5919788
    Abstract: The present invention concerns the compounds of formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dashed line designates an optional bond; R.sup.1 and R.sup.2 are each independently hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; R.sup.3 and R.sup.4 are each independently hydrogen, C.sub.1-6 alkyl, phenyl or phenyl substituted with one, two or three substituents selected from halo, hydroxy, nitro, cyano, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, mercapto, amino, mono- and di(C.sub.1-6 alkyl)-amino, carboxyl, C.sub.1-6 alkyloxycarbonyl and C.sub.1-6 alkylcarbonyl; Alk is C.sub.1-4 alkanediyl; D is a pyrimidinone, piperidone or a benzimidozolidinone; having antipsychotic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: June 27, 1997
    Date of Patent: July 6, 1999
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jan Vandenberk, Ludo Edmond Josephine Kennis, Josephus Carolus Mertens
  • Patent number: 5919790
    Abstract: The present invention relates to compounds that are inhibitors of interleukin-1.beta. converting enzyme that have the Formula II ##STR1## This invention also relates to a method of treatment of stroke, inflammatory diseases, septic shock, reperfusion injury, Alzheimer's disease, shigellosis, and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1.beta. converting enzyme.
    Type: Grant
    Filed: October 2, 1997
    Date of Patent: July 6, 1999
    Assignees: Warner-Lambert Company, BASF Aktiengesellsschaft
    Inventors: Hamish John Allen, Kenneth Dale Brady, Bradley William Caprathe, Paul Galatsis, John Lodge Gilmore, Sheryl Jeanne Hays, Robert Vincent Talanian, Nigel Walker, Joseph Scott Warmus
  • Patent number: 5902814
    Abstract: There are provided new compounds of formula I: ##STR1## wherein R represents hydrogen or methyl; andn represents 1 or 2;or a pharmaceutically acceptable acid addition salt thereof, together with processes for preparing them, compositions containing them and their use in therapy. Compounds of formula I are expected to be useful in the treatment of psychotic disorders, intellectual impairment disorders and anxiety.
    Type: Grant
    Filed: September 18, 1995
    Date of Patent: May 11, 1999
    Assignee: Astra AB
    Inventors: John Charles Gordon, Ronald Conrad Griffith, Robert John Murray, Michael Balestra
  • Patent number: 5869496
    Abstract: Disclosed are spiro-substituted azacycles of formula (I), are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, emesis and asthma. In particular compounds of formula (I) are shown to be neurokinin antagonists.
    Type: Grant
    Filed: July 11, 1995
    Date of Patent: February 9, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Hongbo Qi, Shrenik K. Shah
  • Patent number: 5861409
    Abstract: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.
    Type: Grant
    Filed: April 8, 1997
    Date of Patent: January 19, 1999
    Assignee: Eli Lilly and Company
    Inventors: James E. Audia, Stephen Richard Baker, Jesus Ezquerra Carrera, Carlos Lamas Peteira, Concepcion Pedregal Tercero
  • Patent number: 5807865
    Abstract: The present invention relates to compounds of the formula (I) ##STR1## wherein X, Z, R, R.sup.1, R.sup.2, Ar, n and m are as defined herein which are of use in the treatment or prevention of neuropathy, asthma, osteoarthritis, rheumatoid arthritis or migraine.
    Type: Grant
    Filed: October 18, 1996
    Date of Patent: September 15, 1998
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Timothy Harrison, Christopher John Swain
  • Patent number: 5808071
    Abstract: A commercial scale process for the production of tetrahydroisoquinolines and related heterocyclics by reaction, in mildly acidic conditions, of aryl N-sulfonylethylamines in the presence of a suitable Lewis acid, and a compound capable of in situ generation of formaldehyde. The process is further characterized by formaldehyde being generated by the reaction of the Lewis acid upon the formaldehyde generating agent, instead of being present as an initial reactant. The process further avoids the presence of initial water which destroys the Lewis acid before it can act upon the formaldehyde generating agent.
    Type: Grant
    Filed: July 15, 1997
    Date of Patent: September 15, 1998
    Assignee: Hoechst Marion Roussell, Inc.
    Inventor: Timothy James-Norman Watson
  • Patent number: 5786481
    Abstract: 3,7-Diazabicyclo?3.3!nonanes and selected derivatives thereof of the general formula: ##STR1## wherein Q=S; Z=CH.sub.2 ; and Y equals an N-acyl or N-alkyl group are disclosed as multiclass antiarrhythmic agents.
    Type: Grant
    Filed: October 19, 1995
    Date of Patent: July 28, 1998
    Assignee: The Board of Regents, Oklahoma State University
    Inventors: Kenneth Darrell Berlin, Gregory Lynn Garrison, Subbiah Sangiah, Cyril Roy Clarke, Chun-Lin Chen, Ralph Lazzara, Benjamin Jacob Scherlag, Eugene Stuart Patterson, George Edward Burrows
  • Patent number: 5756743
    Abstract: Novel spiro?cyclopent?b!indole-piperidines!, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the spiro?cyclopent?b!indole-piperidines! and intermediates, or compositions thereof are disclosed.
    Type: Grant
    Filed: February 18, 1997
    Date of Patent: May 26, 1998
    Assignee: Hoechst Marion Roussel Inc.
    Inventors: Mark G. Palermo, Gerard J. O'Malley
  • Patent number: 5750533
    Abstract: There are disclosed 14.alpha.-hydroxymarcfortine derivatives of the natural products marcfortine A, B, C, and D useful in the treatment and prevention of helminth and arthropod infections of animals and plants. The synthetic derivatives are of Formula (I).
    Type: Grant
    Filed: December 7, 1995
    Date of Patent: May 12, 1998
    Assignee: Pharmacia & Upjohn Company
    Inventor: Byung H. Lee
  • Patent number: 5731441
    Abstract: The invention provides hydroxamic acid derivatives of the general formula ##STR1## wherein R.sup.1 represents cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; R.sup.2 represents a saturated 5- to 8-membered monocyclic or bridged N-heterocyclic ring, which N-heterocyclic ring is attached via the N atom and when it is monocyclic, optionally contains NR.sup.4, O, S, SO or SO.sub.2 as a ring member and/or is optionally substituted on one or more C atoms by hydroxy, lower alkyl, lower alkoxy, oxo, ketalized oxo, amino, mono(lower alkyl)amino, di(lower alkyl)amino,carboxy, lower alkoxycarbonyl, hydroxy-methyl, lower alkoxymethyl, carbamoyl, mono(lower alkyl)-carbamoyl, di(lower alkyl)carbamoyl or hydroxyimino; R.sup.3 represents a 5- or 6-membered N-heterocyclic ring which (a) is attached via the N atom, (b) optionally contains N, O and/or S, SO or SO.sub.
    Type: Grant
    Filed: October 29, 1996
    Date of Patent: March 24, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael John Broadhurst, Paul Anthony Brown, William Henry Johnson
  • Patent number: 5723616
    Abstract: The present invention is directed to a novel process for the preparation of the compound N-?1(R)-?(1,2-dihydro-1-methanesulfonyl-spiro?3H-indole-3,4'-piperdin!-1'- yl)carbonyl!-2-(phenylmethyl-oxy)ethyl!-2-amino-2-methyl-propanamide, and salts thereof, which has the structure: ##STR1## and which has the ability to stimulate the release of natural or endogenous growth hormone. This compound may be used to treat conditions which require the stimulation of growth hormone production or secretion such as in humans with a deficiency of natural growth hormone or in animals used for food or wool production where the stimulation of growth hormone will result in a larger, more productive animal.
    Type: Grant
    Filed: October 23, 1996
    Date of Patent: March 3, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Peter G. Houghton, Audrey Molina, Joannis Houpis, Joseph E. Lynch, Ralph P. Volante
  • Patent number: 5684012
    Abstract: This subject invention relates to dimeric 4-phenylpiperidine, 4-phenyl-1,2,3,6-tetrahydropyridine, or 4-phenylpiperazine compounds or dimeric spirocyclic piperidine compounds having general formula (I), ##STR1## wherein n is 1-5; R.sup.1 to R.sup.4 are substituents; R.sup.5 and R.sup.6 each hydrogen or alkyl or form together an ethylene or propylene bridge; X is O, S, SO, SO.sub.2, CO or (CH.sub.2).sub.m, being 0 or 1, X is NR.sup.7, R.sup.7 being H, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, or phenylalkyl, or X is CR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 are selected from hydroxy and the substituents defined under R.sup.7 ; and (i) Z.sup.1 is a substituent and Z.sup.2 is (CH.sub.2).sub.p wherein p is 0; and Y is N, C or CH; (ii) Z.sup.1 and Y are linked together via a single bond, thereby forming a spirocyclic junction; in which case Y is C; Z.sup.1 is O, S, (CH.sub.2).sub.q, q being 1, 2 or 3, or Z.sup.1 is CH.sub.2 O, CH.sub.2 S, CH.sub.2 CH.sub.2 O, CH.sub.2 CH.sub.2 S, CH.dbd.CH, CH.dbd.CHCH.sub.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 4, 1997
    Assignee: H. Lundbeck A/S
    Inventors: Jens Perregaard, John W. Stenberg, Ejner K. Moltzen
  • Patent number: 5654314
    Abstract: The new compounds of formulaA--O--CO--Z (I)(wherein A and Z are defined as explained in the specification) can be prepared by conventional methods; they are suitable as active substances for pharmaceutical compositions.
    Type: Grant
    Filed: March 28, 1995
    Date of Patent: August 5, 1997
    Assignee: Boehringer Ingelheim KG
    Inventors: Rolf Banholzer, Rudolf Bauer, Richard Reichl
  • Patent number: 5637709
    Abstract: Polychromatic compounds of pyrans having a substituted adamantane or a polycyclic ring system, with the exception of adamantane, in the 2-position of the pyran ring, having the structure ##STR1## whereby the residues R.sub.1 -R.sub.4 are independently substituents selected from the series H, alkyl, substituted phenyl, phenyl, naphthyl, OH, alkoxy (C.sub.1 -C.sub.4), halogen, alkylamino, dialkylamino, cyan, trifluormethyl, or, R.sub.1 and R.sub.2 or R.sub.3 and R.sub.4 or R.sub.2 and R.sub.3 are constituents of at least one condensed aromatic, heteroaromatic or an alkane ring, wherein said heteroaromatic ring is selected from the group consisting of pyridine, pyrimidine, pyridazine, quinoline, isoquinoline, naphthyridine, quinazoline, quinoxaline, phthalazine, pteridine, phenazine, and benzoquinoline which are substituted by the same residues as R.sub.1 -R.sub.
    Type: Grant
    Filed: February 9, 1995
    Date of Patent: June 10, 1997
    Assignee: Optische Werke G. Rodenstock
    Inventor: Manfred Melzig
  • Patent number: 5635511
    Abstract: The use of 3,7,9,9-tetrasubstituted 3-phenylsulfonyl-3,7-diazabicyclo[3.3.1]nonane compounds for treating cardiac arrhytmias in larger mammals, including humans; novel antiarrhythmically active 3,7,9,9-tetrasubstituted compounds corresponding to the general formula Ia ##STR1## in which R.sup.1 is an alkyl group having 1-6 carbon atoms or a cycloalkylalkyl group having 4-7 carbon atoms,R.sup.2 is lower alkyl, andR.sup.3 is lower alkyl, orR.sup.2 and R.sup.3 together form an alkylene chain having 3-6 carbon atoms,R.sup.4' is cyano, an R.sup.6 --O--CO-- group in which R.sup.6 is lower alkyl, an R.sup.7 --SO.sub.2 --NH-- group in which R.sup.7 is lower alkyl, or an R.sup.8 --CO--NH-- group in which R.sup.8 is lower alkyl or a phenyl group which is optionally substituted by halogen, cyano, nitro, or an R.sup.9 --SO.sub.2 -- radical in which R.sup.9 is lower alkyl, or an imidazolyl radical located in position 4 of the phenyl ring, andR.sup.
    Type: Grant
    Filed: January 31, 1996
    Date of Patent: June 3, 1997
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Uwe Schoen, Arman Farjam, Reinhard Brueckner, Dieter Ziegler
  • Patent number: 5633248
    Abstract: A compound of the formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 independently represent an optionally substituted aromatic group; P and Q independently represent a divalent aliphatic hydrocarbon group having at least 2 carbon atoms and optionally having either oxygen or sulfur in the carbon chain; R.sup.1 and R.sup.3 independently represent --CO--R, --CONH--R (R represents a hydrocarbon group or a heterocyclic group) or a hydrocarbon group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4, taken together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic group; and j represents 0 or 1, or a salt thereof, has excellent GnRH-receptor antagonizing activity and is useful as a prophylactic and therapeutic agent for hormone-dependent and other diseases.
    Type: Grant
    Filed: November 21, 1995
    Date of Patent: May 27, 1997
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato
  • Patent number: 5629317
    Abstract: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: May 13, 1997
    Assignee: Eli Lilly and Company
    Inventors: James E. Audia, Stephen R. Baker, Jesus E. Carrera, Carlos L. Peteira, Concepcion P. Tercero
  • Patent number: 5610163
    Abstract: Compounds of the formula ##STR1## of which, in exemplary compounds, the thienyl group is attached via the 2-position and:(a) A is 3.alpha.-(6.beta., 7.beta.-epoxy)-tropanyl methobromide and R.sub.1 is 2-thienyl;(b) A is 3.alpha.-(6, 7dehydro)-tropanyl methobromide and R.sub.1 is 2-thienyl;(c) A is 3.beta.-tropanyl methobromide and R.sub.1 is 2-thienyl; and,(d) A is 3.alpha.-(N-isopropyl)-nortropanyl methobromide and R.sub.1 is cyclopentyl.These are anticholinergics. Administered by inhalation, they are useful for the treatment of chronic obstructive bronchitis or slight to moderately severe asthma. Administered by the intravenous or oral routes, they are useful for the treatment of vagally induced sinus bradycardia.
    Type: Grant
    Filed: March 16, 1995
    Date of Patent: March 11, 1997
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Rolf Banholzer, Rudolf Bauer, Richard Reichl
  • Patent number: 5578593
    Abstract: There are disclosed certain novel compounds identified as spiro piperidines and homologs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such spiro compounds as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: November 3, 1993
    Date of Patent: November 26, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Meng-Hsin Chen, David B. R. Johnston, Ravi P. Nargund, Arthur A. Patchett, James R. Tata, Lihu Yang
  • Patent number: 5571918
    Abstract: A method for producing 2-methylspiro(1,3-oxathiolane-5,3')quinuclidine, which comprises reacting 3-hydroxy-3-mercaptomethylquinuclidine or a salt thereof and a carbonyl compound in the presence of a catalyst made of at least one member selected from the group consisting of tin halides, oxyacids of phosphorus, phosphorus oxyhalides and organic sulfonic acids, to produce cis-form 2-methylspiro(1,3-oxathiolane-5,3')quinuclidine or a salt thereof.
    Type: Grant
    Filed: May 11, 1995
    Date of Patent: November 5, 1996
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventors: Koji Hayashi, Sho Tokumoto, Hiroshi Yoshizawa, Tatsuo Isogai, Masaru Kimura, Masahiko Sawaki, Takayoshi Ando, Isamu Katsuyama, Hayato Ariyoshi, Tadashi Nakamura
  • Patent number: 5567624
    Abstract: A composition for determining pH of a solution comprises a fluorescent carbazine dye covalently bound to a solid support. A method of determining pH of a solution comprises placing the composition in the solution, contacting the composition with a selected wavelength of light to excite fluorescence by the carbazine dye, measuring intensities of the fluorescence at two selected wavelengths, calculating a ratio of fluorescence intensities at the two selected wavelengths, and correlating the ratio with a predetermined relationship of such ratios to pH. A fiber optic system for measuring pH of a solution with the carbazine-dye-containing composition is also disclosed.
    Type: Grant
    Filed: April 27, 1995
    Date of Patent: October 22, 1996
    Assignee: Utah Medical Products, Inc.
    Inventor: Roger E. Smith
  • Patent number: 5554620
    Abstract: Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment of neurodegenerative disorders or neurotoxic injuries utilizing them, wherein the substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts have the formula: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X and p are as defined in the specification.
    Type: Grant
    Filed: July 29, 1994
    Date of Patent: September 10, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: Diane L. DeHaven-Hudkins, John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
  • Patent number: 5547958
    Abstract: 8.alpha.-acylamino ergolines are useful dopamine agonists.
    Type: Grant
    Filed: December 27, 1994
    Date of Patent: August 20, 1996
    Assignee: Schering Aktiengesellschaft
    Inventors: Gerhard Sauer, Thomas Brumby, Helmut Wachtel, Jonathan Turner, Peter-Andreas Loschmann
  • Patent number: 5545834
    Abstract: Methods are disclosed for determining an analyte in a medium suspected of containing the analyte. One method comprises providing (1) combining a medium suspected of containing the analyte and a novel chemiluminescent compound, (2) combining a means for chemically activating the chemiluminescent compound; and (3) detecting the amount of luminescence generated by the chemiluminescent compound. The amount of luminescence generated is related to the amount of analyte in the medium. The chemiluminescent compound can be chemically activated by hydrogen peroxide. Compositions and kits are also disclosed.
    Type: Grant
    Filed: January 17, 1995
    Date of Patent: August 13, 1996
    Assignee: Behringwerke AG
    Inventors: Sharat Singh, Rajendra Singh, Frank Meneghini, Edwin F. Ullman
  • Patent number: 5536716
    Abstract: There are disclosed certain novel compounds identified as spiro piperidines and homologs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such spiro compounds as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: November 3, 1993
    Date of Patent: July 16, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Meng-Hsin Chen, David B. R. Johnston, Ravi P. Nargund, Arthur A. Patchett, James R. Tata, Lihu Yang
  • Patent number: 5532255
    Abstract: Compounds of the formula ##STR1## in which R.sup.1, X and Y have the meanings defined herein, and their salts, inhibit the binding of fibrinogen to the fibrinogen receptor and can be used for treating thrombosis, stroke, cardiac infarction, inflammations, arteriosclerosis, osteoporosis and tumors.
    Type: Grant
    Filed: April 29, 1994
    Date of Patent: July 2, 1996
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Peter Raddatz, Joachim Gante, Horst Juraczyk, Hanns Wurziger, Helmut Prucher, Sabine Bernotat-Danielowski, Guido Melzer
  • Patent number: 5532361
    Abstract: Photochromic compounds belonging to the class of spiro-pyrans, having the general formula (I): ##STR1##
    Type: Grant
    Filed: May 12, 1994
    Date of Patent: July 2, 1996
    Assignee: Ministero Dell `Universita` E Della Ricerca Scientifica E Technologica
    Inventors: Pietro Allegrini, Nereo Nodari, Vincenzo Malatesta, Luciana Crisci
  • Patent number: 5527912
    Abstract: 2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula ##STR1## wherein Q is S or CH.dbd.CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y.sup.1 are taken together and are arylmethylene or aralkylmethylene (or a corresponding epoxy derivative) or Y and Y.sup.1 are taken separately and Y is hydrogen or OH, and Y.sup.1 is aryl, aralkyl, arylthio, or aryloxy; and structurally related 2-(piperidino) alkanols; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.
    Type: Grant
    Filed: March 27, 1995
    Date of Patent: June 18, 1996
    Assignee: Pfizer Inc.
    Inventor: Bertrand L. Chenard
  • Patent number: 5498614
    Abstract: The invention relates to bridged aza-bicyclic derivatives of formula (I). These compounds are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders. Also disclosed are intermediates used in the synthesis of compound of formula (I).
    Type: Grant
    Filed: November 7, 1994
    Date of Patent: March 12, 1996
    Assignee: Pfizer Inc.
    Inventor: Manoj C. Desai
  • Patent number: 5493029
    Abstract: The present invention relates to novel benzopyran derivatives of formula (I) which have exellent effectiveness in the treatment of asthma as well as hypertension. ##STR1## wherein: R.sub.1 is --CN, --NO.sub.2, --OCX.sub.1 X.sub.2 X.sub.3, --NH.sub.2, --NHSO.sub.2 R.sup.A, ##STR2## --SO.sub.2 R.sup.C or --SO.sub.2 NR.sup.C R.sup.D wherein X.sub.1, X.sub.2 and X.sub.3 are, each independently, F, Cl or H, except for that X.sub.1, X.sub.2 and X.sub.3 may not be hydrogen atom simulaneously; R.sup.A and R.sup.B are, each independently, a hydrogen atom, or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group; and R.sup.C and R.sup.D are, each independently, a hydrogen atom or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group;R.sub.2 is a C.sub.1-4 straight or branched alkyl group;R.sub.3 is a C.sub.
    Type: Grant
    Filed: December 9, 1993
    Date of Patent: February 20, 1996
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Sung-Eun Yoo, Kyu Y. Yi, Nak C. Jeong, Jee H. Suh, Seon-Ju Kim, Hwa-Sup Shin, Byung H. Lee, Kyu S. Jung
  • Patent number: 5484923
    Abstract: The present invention is directed to a process of making spirocycles of general structural formula: ##STR1## where R.sub.1 is selected from the group consisting of CO--C.sub.1-3 alkyl, cyano, carboxy, carboxy C.sub.1-6 alkyl ester, carboxamide, C.sub.1-6 alkyl sulfinyl, C.sub.1-6 alkyl sulfonyl, C.sub.1-6 methanesulfonamide and halogen; R.sub.2 is selected from the group consisting of keto or alcohol, R.sub.3 is cyano, resulting in compounds which are Class III antiarrhythmic.
    Type: Grant
    Filed: May 31, 1994
    Date of Patent: January 16, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Dongwei Cai, Richard Desmond, Yao-Jun Shi, David M. Tschaen, Thomas R. Verhoeven
  • Patent number: 5472968
    Abstract: Compounds of formula (I), ##STR1## in which R.sub.1 and R.sub.2, which may be the same or different, represent hydrogen, C.sub.1-6 alkyl, R.sub.3 and R.sub.4 independently represent one or more radicals selected from hydrogen, OH, NH.sub.2, NO.sub.2, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy and n is an integer from 1-2 inclusive, and pharmaceutically acceptable derivatives thereof are useful as pharmaceuticals; in particular, they possess N-methyl-(d)-aspartate(NMDA) blocking properties and are useful in the treatment and/or prevention of neurodegenerative conditions.
    Type: Grant
    Filed: March 16, 1993
    Date of Patent: December 5, 1995
    Assignee: Fisons Corporation
    Inventors: Ronald C. Griffith, James R. Matz, James J. Napier
  • Patent number: 5468858
    Abstract: 3,7-Diazabicyclo[3.3.1]nonanes and selected derivatives thereof of the general formula: ##STR1## are disclosed as multiclass antiarrhythmic agents.
    Type: Grant
    Filed: October 28, 1993
    Date of Patent: November 21, 1995
    Assignee: The Board of Regents of Oklahoma State University Physical Sciences
    Inventors: Kenneth D. Berlin, Gregory L. Garrison, Subbiah Sangiah, Cyril R. Clarke, Chun-Lin Chen, Ralph Lazzara, Benjamin J. Scherlag, Eugene S. Patterson, George E. Burrows
  • Patent number: 5414088
    Abstract: The invention concerns compounds of formula I ##STR1## where R.sup.1 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.3 -C.sub.7 -cycloalkyl, R.sup.2 is C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, cyano, carboxy [carbonyl substituted by hydroxyl], C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino or hydrazino or R.sup.1 and R.sup.2 together are C.sub.2 -C.sub.6 -alkylidene or C.sub.3 -C.sub.6 -cycloalkylidene or R.sup.1 and R.sup.2, together with the carbon atoms to which they are attached, form a C.sub.3 -C.sub.7 -spirocycle, n is 0 or 1, R.sup.3 is hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, C.sub.3 -C.sub.7 -cycloalkyl, benzyl, carboxy-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkyloxycarbonyl-C.sub.1 -C.sub.6 -alkyl or di-C.sub.1 -C.sub.6 -alkyloxophosphinyl-C.sub.1 -C.sub.6 -alkyl and R.sup.4 -R.sup. 6 are as in the specification.
    Type: Grant
    Filed: April 14, 1992
    Date of Patent: May 9, 1995
    Assignee: Boehringer Mannheim GmbH
    Inventors: Wolfgang Von Der Saal, Harald Zilch, Erwin Bohm
  • Patent number: 5391748
    Abstract: The present invention relates to dihydroquinolines of formula (I): ##STR1## in which the symbols used are as defined in the description, to a process for their preparation, to their use in recording materials and to recording materials in which such dihydroquinolines are present.
    Type: Grant
    Filed: December 3, 1993
    Date of Patent: February 21, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventor: Horst Berneth
  • Patent number: 5391742
    Abstract: 2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula ##STR1## wherein Q is S or CH.dbd.CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y.sup.1 are taken together and are arylmethylene or aralkylmethylene (or a corresponding epoxy derivative) or Y and Y.sup.1 are taken separately and Y is hydrogen or OH, and Y.sup.1 is aryl, aralkyl, arylthio, or aryloxy; and structurally related 2-(piperidino)alkanols; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.
    Type: Grant
    Filed: April 15, 1994
    Date of Patent: February 21, 1995
    Assignee: Pfizer Inc.
    Inventor: Bertrand L. Chenard
  • Patent number: 5369084
    Abstract: Isonicotinic acid derivatives and related furo-, thieno- and pyrrolo[3,4-c]pyridin-1(3H)-one, -thione and -imine compounds having the formula ##STR1## wherein R is ##STR2## Q is O, S or NR.sup.7 ; Y is O, S or NR.sup.8 ; L is COOR.sup.9, CONR.sup.10 R.sup.11, C(.dbd.S)NR.sup.10 R.sup.11, CN, or a radical of formula ##STR3## the acceptable addition salts, the stereochemically isomeric forms and the N-oxides thereof, having herbicidal properties, compositions containing the same and methods for controlling weeds.
    Type: Grant
    Filed: May 6, 1993
    Date of Patent: November 29, 1994
    Assignee: Janssen Pharmaceutical N.V.
    Inventors: Hans-Rudolf Waespe, Guy R. E. Van Lommen, Victor K. Sipido
  • Patent number: 5332746
    Abstract: The invention relates to a group of new 8,9-annelated-.beta.-carbolines and 8,9-annelated-3,4-dihydro-.beta.-carbolines having interesting fibrinolytic properties. In particular the compounds can be used as orally active fibrinolytics.The compounds have the general formulae 1 and 2 ##STR1## wherein R.sub.2 +R.sub.3 together with the carbon atom and the nitrogen atom to which they are bound and the intermediate carbon atom constitute a heterocyclic group consisting of 5-10 ring atoms.
    Type: Grant
    Filed: May 8, 1991
    Date of Patent: July 26, 1994
    Assignee: Duphar International Research B.V.
    Inventors: Derk Hamminga, Hans H. Haeck, Ineke van Wijngaarden, Johannes W. C. M. Jansen
  • Patent number: 5324732
    Abstract: 1.5 Fumaric acid salts of N,N'-di-lower alkyl-substituted 9,9-alkylene-3,7-diazabicyclo[3.3.1 ]nonanes and a process for obtaining them in stoichiometrically pure and virtually non-hygroscopic form.
    Type: Grant
    Filed: November 23, 1992
    Date of Patent: June 28, 1994
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Uwe Schoen, Walter Heitmann, Uwe Maetzel
  • Patent number: 5300511
    Abstract: The present invention relates to novel benzopyran derivatives of formula(I) which have exellent effectiveness in the treatment of asthma as well as hypertension. ##STR1## wherein R.sub.1 is --CN, --NO.sub.2, --OCX.sub.1 X.sub.2 X.sub.3, --NH.sub.2, --NHSO.sub.2 R.sup.A, ##STR2## --SO.sub.2 R.sup.C or --SO.sub.2 NR.sup.C R.sup.D wherein X.sub.1, X.sub.2 and X.sub.3 are, each independently, F, Cl or H, except for that X.sub.1, X.sub.2 and X.sub.3 may not be hydrogen atom simulaneously; R.sup.A and R.sup.B are, each independently, a hydrogen atom, or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group; and R.sup.C and R.sup.D are, each independently, a hydrogen atom or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group;R.sub.2 is a C.sub.1-4 straight or branched alkyl group;R.sub.3 is a C.sub.
    Type: Grant
    Filed: May 21, 1992
    Date of Patent: April 5, 1994
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Sung-Eun Yoo, Kyu Y. Yi, Nak C. Jeong, Jee H. Suh, Seon-Ju Kim, Hwa-Sup Shin, Byung H. Lee, Kyu S. Jung
  • Patent number: 5292747
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X, m, n, p, and q are as set forth in the specification, as well as pharmaceutically acceptable salts of acidic compounds of formula I with bases and of basic compounds of formula I with acids, which are useful in the control or prevention of inflammatory, immunological, oncological, bronchopulmonary, dermatological or cardiovascular disorders or for the treatment of asthma, AIDS or diabetic complications or for the stimulation of hair growth are described.
    Type: Grant
    Filed: September 21, 1992
    Date of Patent: March 8, 1994
    Assignee: Hoffman-La Roche Inc.
    Inventors: Peter D. Davis, Christopher H. Hill, Goeffrey Lawton
  • Patent number: 5292746
    Abstract: The present invention is directed to a new class of cyclic nitrones and their use as spin trapping agents.
    Type: Grant
    Filed: August 5, 1992
    Date of Patent: March 8, 1994
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Albert A. Carr, Craig E. Thomas, Ronald C. Bernotas, George Ku
  • Patent number: 5281710
    Abstract: A fused ring system compound is disclosed that contains an epoxide group on one side of the fused rings and an enediyne macrocyclic ring on the other side of the fused rings. The compounds have DNA-cleaving, antimicrobial and tumor growth-inhibiting properties. Chimeric compounds having the fused ring system compound as an aglycone bonded to (i) a sugar moiety as the oligosaccharide portion or (ii) a monoclonal antibody or antibody combining site portion thereof that immunoreacts with target tumor cells are also disclosed. Compositions containing a compound or a chimer are disclosed, as are methods of preparing a compound.
    Type: Grant
    Filed: September 1, 1992
    Date of Patent: January 25, 1994
    Assignee: The Scripps Research Institute
    Inventors: Adrian L. Smith, Chan-Kou Hwang, Sebastian V. Wenderborn, Kyriacos C. Nicolaou, Erwin P. Schreiner, Wilhelm Stahl, Wei-Min Dai, Peter E. Maligres, Toshio Suzuki
  • Patent number: 5254564
    Abstract: A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring and R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, preferably methyl or ethyl, .sup.4 or phenyl, or R.sub.3 together with R.sub.1 forms a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, group;R.sub.4 and R.sub.5 are identical and are hydrogen or C.sub.1-6 alkyl, or together form a C.sub.2-5 linear polymethylene group; R.sub.6 and R.sub.7 are identical and are hydrogen or C.sub.1-6 alkyl, or together form a C.sub.2-5 linear polymethylene group;or R.sub.5 and R.sub.6 are together --CH.sub.2 -- when each of R.sub.4 and R.sub.7 is hydrogen or C.
    Type: Grant
    Filed: July 16, 1990
    Date of Patent: October 19, 1993
    Assignee: Lo Zambeletti S.p.A.
    Inventors: Vittorio Vecchietti, Giuseppe Giardina, Roberto Colle
  • Patent number: 5227488
    Abstract: Indole derivatives of formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be hydrogen or lower alkyl optionally substituted by halogen; X represents oxygen or sulfur; A.sup.1 represents a straight or branched alkylene chain containing from 2 to 4 carbon atoms; R.sup.5 is hydrogen or a straight or branched alkyl group; A.sup.2 is a straight or branched, saturated or unsaturated hydrocarbon chain containing from 2 to 6 carbon atoms; and R.sup.6 is selected from a group consisting of various structures, have been found to exhibit central nervous system activities.
    Type: Grant
    Filed: September 28, 1990
    Date of Patent: July 13, 1993
    Assignee: Novo Nordisk A/S
    Inventors: Lone Jeppesen, Peter H. Andersen, Louis B. Hansen, Peter Faarup, John B. Hansen